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Synthesis and characterization of folic acid modified water-soluble chitosan derivatives for folate-receptor-mediated targeting

  作者 Jing, HH; Guo, ZD; Guo, WY; Yang, WJ; Xu, P; Zhang, XZ  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-10;  页码  3418-3424  
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[摘要]Three chemical modification methods of carboxymethylation, quaternization and hydroxypropylation were used to synthesize water-soluble chitosan derivatives. In order to study the feasibility of these chitosan derivatives as backbones of nuclear imaging agents, folic acid (FA) and Technetium-99m were introduced onto the water-soluble chitosan chains. The bifunctional chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was conjugated to the folate grafted chitosan derivatives for chelating with radionuclides such as Cu-64 and Ga-68. The structures of these new ligands were characterized with multiple methods. The solubility and stability of the Tc-99m-complexes were both favorable. Further study of their radiochemical and biological properties will be performed to evaluate the usefulness of these water-soluble chitosan derivatives for nuclear imaging agent design. (C) 2012 Elsevier Ltd. All rights reserved.

 
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